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SML0796

HI-TOPK-032

≥98% (HPLC)

别名:

N-(12-氰基吲哚并[2,3-b]喹喔啉-2-基)-2-噻吩甲酰胺

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关于此项目

经验公式（希尔记法）:
C20H11N5OS
化学文摘社编号:
487020-03-1
分子量:
369.40
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
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Quality Level

100

assay

≥98% (HPLC)

form

powder

color

orange to dark red

solubility

DMSO: 3 mg/mL, clear (warmed)

storage temp.

2-8°C

SMILES string

[s]1c(ccc1)C(=O)Nc2cc3[n](c4nc5c(nc4c3C#N)cccc5)cc2

InChI

1S/C20H11N5OS/c21-11-13-16-10-12(22-20(26)17-6-3-9-27-17)7-8-25(16)19-18(13)23-14-4-1-2-5-15(14)24-19/h1-10H,(H,22,26)

InChI key

BCSBXWKRZUPFHW-UHFFFAOYSA-N

相关类别

Application

HI-TOPK-032已被用作PDZ结合激酶（PBK）抑制剂。

Biochem/physiol Actions

HI-TOPK-032属于ATP竞争性抑制剂类。它也可以用作大肠癌的有效治疗剂。
HI-TOPK-032是体外和体内的特异性TOPK（源自T-LAK细胞的蛋白激酶）抑制剂。HI-TOPK-032在结肠癌异种移植模型中抑制了肿瘤的生长。
HI-TOPK-032是一款特异性TOPK抑制剂。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000175428
0000175427
0000175428
0000175427
0000053308

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Dong Joon Kim et al.
Cancer research, 72(12), 3060-3068 (2012-04-24)
The serine-threonine mitogen-activated protein kinase kinase family member T-LAK cell-originated protein kinase (TOPK/PBK) is heavily involved in tumor development, cancer growth, apoptosis, and inflammation. Despite the identification of TOPK as a promising novel therapeutic target, no inhibitor of TOPK has
PBK/TOPK enhances aggressive phenotype in prostate cancer via β-catenin-TCF/LEF-mediated matrix metalloproteinases production and invasion.
Brown-Clay J D, et al.
Oncotarget, 6(17), 15594?15609-15594?15609 (2015)
PBK/TOPK mediates geranylgeranylation signaling for breast cancer cell proliferation.
Dou X, et al.
Cancer Cell International, 15(1), 27-27 (2015)
Xiong Zhang et al.
Cancers, 13(7) (2021-05-01)
Metastatic castration-resistant prostate cancer (mCRPC) is a highly aggressive disease with few therapeutic options. Hyperactive androgen receptor (AR) signaling plays a key role in CRPC progression. Previously, we identified RAR-related orphan receptor gamma (RORγ) as a novel key driver of
Xiaoyan Dou et al.
Cancer cell international, 15, 27-27 (2015-03-10)
PDZ binding-kinase (PBK) (also named T-lymphokine-activated killer cell-originated protein kinase (TOPK)), a serine/threonine kinase, is tightly controlled in normal tissues but elevated in many tumors, and functions in tumorigenesis and metastasis. However, the signaling that regulates expression of PBK in

全球贸易项目编号

货号GTIN
SML0796-25MG04061832450933
SML0796-5MG04061832450940

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